中枢神经系统锥虫病的化疗：乙酰氨基苯脒或喷他脒与DL-α-二氟甲基鸟氨酸（DFMO）联合使用。

Chemotherapy of CNS-trypanosomiasis: the combined use of diminazene aceturate or pentamidine with DL-alpha-difluoromethylornithine (DFMO).

作者信息

Jennings F W

机构信息

Department of Veterinary Parasitology, University of Glasgow, Scotland.

出版信息

Trop Med Parasitol. 1992 Jun;43(2):106-9.

PMID:1519020

Abstract

The chemotherapy of CNS-trypanosomiasis with DL-alpha-difluoromethylornithine (Eflornithine, DFMO) with the diamidine, pentamidine (Lomidine) or diminazene aceturate (Berenil) was examined using the mouse model for CNS-trypanosomiasis. Although combined DFMO/pentamidine therapy can give complete cures, one or more doses of 100 mg/kg pentamidine was required with continuous administration of DFMO for 14-16 days, and even this treatment failed to cure the mice in a repeat experiment. Diminazene aceturate was more efficient and provided a 40 mg-kg dose was utilised, it was possible to reduce the period of DFMO to approximately 12 days. Attempts to reduce the dose rate of diminazene to less than 40 mg-kg failed. Of the two compounds, diminazene aceturate was the more successful and could possibly be used in combination with DFMO in the treatment of CNS-trypanosomiasis.

摘要

利用中枢神经系统锥虫病小鼠模型，研究了DL-α-二氟甲基鸟氨酸（依氟鸟氨酸，DFMO）与双脒类药物戊烷脒（洛米定）或乙酰甘氨酸二脒那嗪（贝尼尔）联合用于中枢神经系统锥虫病化疗的情况。虽然DFMO/戊烷脒联合疗法可以实现完全治愈，但在连续给予DFMO 14 - 16天的同时，需要一剂或多剂100mg/kg的戊烷脒，甚至在重复实验中这种治疗也未能治愈小鼠。当使用40mg/kg剂量的乙酰甘氨酸二脒那嗪时效果更佳，并且有可能将DFMO的给药时间缩短至约12天。尝试将乙酰甘氨酸二脒那嗪的剂量率降低至低于40mg/kg未成功。在这两种化合物中，乙酰甘氨酸二脒那嗪更为成功，可能与DFMO联合用于中枢神经系统锥虫病的治疗。